Department of Chemistry, Kyiv National Taras Shevchenko University, Kyiv 01601, Ukraine.
Mol Divers. 2012 Nov;16(4):625-37. doi: 10.1007/s11030-012-9407-9. Epub 2012 Oct 30.
128 Azomethines were synthesized through condensation of carbonyl compounds with various amines in pyridine in the presence of Me(3)SiCl as promoter and water scavenger in 58-98 % yield. Et(3)N was added to reaction mixtures before precipitating the product with H(2)O to prevent acid catalyzed hydrolysis of the C=N bond. The scope and limitation of the method are discussed. High yields and simple setup/workup procedure make this method suitable for the combinatorial synthesis of azomethines, which are suitable as starting materials for high throughput synthesis of various combinatorial libraries. The azomethines synthesized were used as starting materials in a one-pot combinatorial synthesis of amines and amides.
128 种亚甲胺通过在吡啶中羰基化合物与各种胺的缩合反应合成，其中 Me(3)SiCl 为促进剂，水为除水剂，产率为 58-98%。在用水沉淀产物之前，向反应混合物中加入 Et(3)N，以防止 C=N 键被酸催化水解。讨论了该方法的适用范围和局限性。高收率和简单的设置/后处理程序使该方法适用于亚甲胺的组合合成，亚甲胺适合作为各种组合文库高通量合成的起始原料。合成的亚甲胺被用作一锅法组合合成胺和酰胺的起始原料。
